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  • Title: Design and structural analysis of novel pharmacophores for potent and selective peroxisome proliferator-activated receptor gamma agonists.
    Author: Lin CH, Peng YH, Coumar MS, Chittimalla SK, Liao CC, Lyn PC, Huang CC, Lien TW, Lin WH, Hsu JT, Cheng JH, Chen X, Wu JS, Chao YS, Lee HJ, Juo CG, Wu SY, Hsieh HP.
    Journal: J Med Chem; 2009 Apr 23; 52(8):2618-22. PubMed ID: 19301897.
    Abstract:
    Utilizing medicinal chemistry design strategies such as benzo splitting and ring expansion, we converted PPARalpha/gamma dual agonist 1 to selective PPARgamma agonists 19 and 20. Compounds 19 and 20 were 2- to 4-fold better than rosiglitazone at PPARgamma receptor, with 80- to 100-fold PPARgamma selectivity over PPARalpha receptor. X-ray cocrystal studies in PPARgamma and modeling studies in PPARalpha give molecular insights for the improved PPARgamma potency and selectivity for 19 when compared to 1.
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